{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T04:44:46Z","timestamp":1760244286664,"version":"build-2065373602"},"reference-count":22,"publisher":"MDPI AG","issue":"21","license":[{"start":{"date-parts":[[2022,11,2]],"date-time":"2022-11-02T00:00:00Z","timestamp":1667347200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["21877006"],"award-info":[{"award-number":["21877006"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Chemical modification of old drugs is an important way to obtain new ones, and it has been widely used in developing new aminoglycoside antibiotics. However, many of the previous modifying strategies seem arbitrary for their lack of support from structural biological detail. In this paper, based on the structural information of aminoglycoside and its drug target, we firstly analyzed the reason that some 2\u2032-N-acetylated products of aminoglycosides caused by aminoglycoside-modifying enzyme AAC(2\u2032) can partially retain activity, and then we designed, synthesized, and evaluated a series of 2\u2032-modified kanamycin A derivatives. Bioassay results showed our modifying strategy was feasible. Our study provided valuable structure\u2013activity relationship information, which would help researchers to develop new aminoglycoside antibiotics more effectively.<\/jats:p>","DOI":"10.3390\/molecules27217482","type":"journal-article","created":{"date-parts":[[2022,11,3]],"date-time":"2022-11-03T03:53:07Z","timestamp":1667447587000},"page":"7482","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Design, Synthesis, and Bioassay of 2\u2032-Modified Kanamycin A"],"prefix":"10.3390","volume":"27","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-1443-7134","authenticated-orcid":false,"given":"Ribai","family":"Yan","sequence":"first","affiliation":[{"name":"National Demonstration Center for Experimental Pharmacy Education, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiaonan","family":"Li","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yuheng","family":"Liu","sequence":"additional","affiliation":[{"name":"Department of Medical Chemistry, College of Pharmaceutical Science, Hebei Medical University, Shijiazhuang 050017, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xinshan","family":"Ye","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,11,2]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"477","DOI":"10.1021\/cr0301088","article-title":"Molecular Insights into Aminoglycoside Action and Resistance","volume":"105","author":"Magnet","year":"2005","journal-title":"Chem. 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